Apamin

Name: Apamin
Brand: Tocris Bioscience
SKU: 1652
Rating: 5 (1 reviews)

Tocris Bioscience, part of Bio-Techne | Catalog # 1652

(1)

Citations (176)

COA / SDS

KCa2 (SK) channel blocker

Key Product Details

Description:	K_Ca2 (SK) channel blocker
Purity:	≥95% (HPLC)
Molecular Weight:	2027.34

View Full Technical Details for Apamin

Technical Data
Citations / Reviews (1)

Biological Activity for Apamin

Apamin is a potent and highly selective inhibitor of small-conductance Ca²⁺-activated K⁺-channels (K_Ca2, SK) (IC₅₀ values are 87.7 pM, 2.3 nM and 4.1 nM for K_Ca2.2, K_Ca2.3 and K_Ca2.1 channels, respectively). Reduces release and mRNA expression of inflammatory cytokines TNFα and IL-6. In models of kidney and cardiovascular disease apamin ameliorates tissue injury and dysfunction. Brain penetrant, blocks medium after-hyperpolarization in vitro, reduces neuroinflammation, increases microglia node contacts and Purkinje cell instananeous firing frequency.

Technical Data for Apamin

M. Wt	2027.34
Formula	C₇₉H₁₃₁N₃₁O₂₄S₄
Single Letter Sequence	CNCKAPETALCARRCQQH (Modifications: Disulfide bridges: 1-11, 3-15, His-18 = C-terminal amide)
Storage	Store at -20°C
Purity	≥95% (HPLC)
CAS Number	24345-16-2
PubChem ID	16133797
InChi Key	YVIIHEKJCKCXOB-STYWVVQQSA-N
Smiles	[H]N[C@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](C)NC2=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC2=CNC=N2)C(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O)[C@@H](C)O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Apamin

Solubility

Soluble to 1mg/ml in water

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References for Apamin

References are publications that support the biological activity of the product.

Kim Antioxidative, antiapoptotic, and anti-inflammatory effects of apamin in a murine model of lipopolysaccharide-induced acute kidney injury. Molecules 2020 PMID: 33287398
Ronzano Microglia-neuron interaction at nodes of Ranvier depends on neuronal activity through potassium release and contributes to remyelination. Nat.Commun. 2021 PMID: 34471138
van der Staay Behavioral effects of apamin, a selective inhibitor of the SK_Ca-channel, in mice and rats. Neurosci.Biobehav.Rev. 1999 PMID: 10643819
Strong Potassium channel toxins. Pharmacol.Ther. 1990 PMID: 2181489
Stocker Matching molecules to function: neuronal Ca²⁺-activated K⁺ channels and afterhyperpolarizations. Toxicon 2004 PMID: 15208027
Habermann Apamin. Pharmacol.Ther. 1984 PMID: 6095335